Dosage form containing (s)-pantoprazole as active ingredient

Abstract

Dosage forms for the oral administration of the magnesium salt of (S)-pantoprazole are described.

1 . A dosage form for oral administration of (S)-pantoprazole magnesium salt comprising a therapeutically effective amount of the (S)-pantoprazole magnesium salt together with pharmaceutically acceptable excipients.  
   
   
       2 . The dosage form according to  claim 1 , which is a solid dosage form in tablet or pellet form.  
   
   
       3 . The dosage form according to  claim 1 , which is a delayed release dosage form comprising an enteric layer, which is soluble in neutral or alkaline conditions and at least one intermediate layer.  
   
   
       4 . The dosage form according to  claim 1 , wherein the (S)-pantoprazole magnesium salt is (S)-pantoprazole magnesium dihydrate.  
   
   
       5 . The dosage form according to  claim 1 , which is an orally administerable medicament in pellet or tablet form which is resistant to gastric juice, and in which each pellet or tablet comprises a core in which active compound or its physiologically-tolerated salt is in admixture with binder, filler and, optionally, a member selected from the group consisting of another tablet auxiliary, a basic physiologically-tolerated inorganic compound, an inert water-soluble intermediate layer surrounding the core and an outer layer which is resistant to gastric juice, wherein the active compound is (S)-pantoprazole magnesium dihydrate, the binder is polyvinylpyrrolidone and/or hydroxypropylmethylcellulose and the filler is mannitol.  
   
   
       6 . The dosage form according to  claim 5  in tablet form, wherein polyvinylpyrrolidone and/or hydroxypropylmethylcellulose is the binder and mannitol is the filler.  
   
   
       7 . The dosage form according to  claim 5  in pellet form, wherein polyvinylpyrrolidone and/or hydroxypropylmethylcellulose is the binder.  
   
   
       8 . The dosage form according to  claim 5 , wherein a pharmacologically tolerated alkali metal, alkaline earth metal or earth metal salt of a weak acid or pharmacologically tolerated hydroxide or oxide of an alkaline earth or earth metal is the basic, physiologically tolerated inorganic compound.  
   
   
       9 . The dosage form according to  claim 8 , wherein sodium carbonate is the basic, physiologically tolerated inorganic compound.  
   
   
       10 . The dosage form according to  claim 1 , comprising low molecular weight polyvinylpyrrolidone as binder and one or more other suitable pharmaceutical excipients.  
   
   
       11 . The dosage form according to  claim 10 , wherein the low molecular weight polyvinylpyrrolidone has an average molecular weight below 70,000.  
   
   
       12 . The dosage form according to  claim 10 , wherein the low molecular weight polyvinylpyrrolidone has an average molecular weight below 60,000.  
   
   
       13 . The dosage form according to  claim 10 , wherein the low molecular weight polyvinylpyrrolidone has an average molecular weight below 40,000.  
   
   
       14 . The dosage form according to  claim 1 , comprising the (S)-pantoprazole magnesium salt together with polyvinylpyrrolidone in an alkaline pellet or tablet core.  
   
   
       15 . The dosage form according to  claim 14 , comprising at least one subcoating and an outer enteric layer, which is soluble in the small intestine.  
   
   
       16 . The dosage form according to  claim 1 , in tablet form, comprising as excipients for the tablet core sodium carbonate, mannitol, crospovidone, polyvinylpyrrolidone, and magnesium stearate.  
   
   
       17 . The dosage form according to  claim 1 , in tablet form, comprising as excipients for the tablet core sodium carbonate, mannitol, crospovidone, polyvinylpyrrolidone, and calcium stearate.  
   
   
       18 . The oral dosage form in pellet or tablet form for magnesium salt of (S)-pantoprazole comprising a therapeutically effective amount of the magnesium salt of (S)-pantoprazole together with one or more other pharmaceutical excipients in an alkaline pellet or tablet core, at least one subcoating and an outer enteric layer which is soluble in the small intestine.  
   
   
       19 . The dosage form according to  claim 1  containing between 5 and 100 mg, of the magnesium salt of (S)-pantoprazole.  
   
   
       20 . The dosage form according to  claim 19 , which contain an amount of the magnesium salt of (S)-pantoprazole, which corresponds to 10, 20, 40, 50, 80 or 100 mg of (S)-pantoprazole.  
   
   
       21 . The dosage form according to  claim 20 , which contain an amount of the magnesium salt of (S)-pantoprazole, which corresponds to 80 mg of (S)-pantoprazole.  
   
   
       22 . The dosage form according to  claim 1  in pellet form, comprising a pellet core, an intermediate layer and an enteric coating, wherein the pellet core is formed from starter pellets, (S)-pantoprazole magnesium dihydrate, starch and optionally other excipients.  
   
   
       23 . The dosage form according to  claim 22 , wherein the starch is pregelatinized starch.  
   
   
       24 . The dosage form according to  claim 23 , wherein a binder, a basic physiologically-tolerated inorganic compound and a wetting agent are present as additional excipients.  
   
   
       25 . The dosage form according to  claim 24 , wherein PVP, sodium dodecylsulfate and sodium carbonate are present.  
   
   
       26 . The dosage form according to  claim 22  in pellet form, comprising a pellet core an intermediate layer and an enteric coating, wherein the pellet core is formed from sucrose starter pellets, (S)-pantoprazole magnesium dihydrate, sodium carbonate, PVP 25, pregelatinized starch and sodium dodecylsulfate, the intermediate layer is formed of HPMC, PVP 25, titanium dioxide and iron oxide yellow, and the enteric coating is formed of Eudragit L 30 D and triethyl citrate.  
   
   
       27 . The dosage form according to  claim 1  in tablet form comprising a tablet core, an intermediate layer and an enteric coating, wherein the tablet core comprises (S)-pantoprazole magnesium dihydrate, sodium carbonate, mannitol, crospovidone, PVP 90 and calcium stearate, the intermediate layer is formed of HPMC, PVP 25, Titanium dioxide, iron oxide yellow and propylene glycol, and the enteric coating is formed of Eudragit L 30 D and triethyl citrate.  
   
   
       28 . A method for the prophylaxis or treatment of a clinical condition in a mammal, such as a human, for which a proton pump inhibitor is indicated, which comprises administration of a therapeutically effective amount (S)-pantoprazole magnesium in a dosage form according to  claim 1 .  
   
   
       29 . The method of treatment according to  claim 28 , wherein the clinical condition is selected from the group consisting of benign gastric ulcer, gastro-oesophageal reflux disease, Zollinger-Ellison syndrome, duodenal ulcer, duodenal ulcer associated with  Helicobacter pylori , and prophylaxis of NSAID-associated gastric or duodenal ulcer in patients with an increased risk of gastroduodenal complication who require continued NSAID treatment and combination therapy with antibiotics in the eradication of  Helicobacter pylori.    
   
   
       30 . The method according to  claim 29 , wherein the clinical condition is gastro-oesophageal reflux disease (GERD).  
   
   
       31 . The method according to  claim 30 , wherein the clinical condition is GERD I to III according to Savary/Miller Classification.  
   
   
       32 . The method according to  claim 30 , wherein the dosage form is an oral dosage form in pellet form, comprising a pellet core an intermediate layer and an enteric coating, wherein the pellet core is formed from sucrose starter pellets, (S)-pantoprazole magnesium dihydrate, sodium carbonate, PVP 25, pregelatinized starch and sodium dodecylsulfate, the intermediate layer is formed of HPMC, PVP 25, titanium dioxide and iron oxide yellow, and the enteric coating is formed of Eudragit L 30 D and triethyl citrate.  
   
   
       33 . The method according to  claim 28 , wherein the effective amount of (S)-pantoprazole magnesium corresponds to 40 or 80 mg pantoprazole.  
   
   
       34 . The method according to  claim 33 , wherein the treatment is a once daily treatment.  
   
   
       35 . The method for production of a dosage form according to  claim 1  in pellet form by spraying a suspension of the magnesium salt of (S)-pantoprazole, starch and optionally other excipients in an aqueous solution of PVP on starter pellets, drying the pellets, and layering them with subcoating and enteric coating.  
   
   
       36 . The method for production according to  claim 36 , wherein the starch is pregelatinized starch.  
   
   
       37 . The method for production of a dosage form according to  claim 1  in pellet form by spraying a suspension of the magnesium salt of (S)-pantoprazole, sodium carbonate, pregelatinized starch and sodium dodecylsulfate in an aqueous solution of PVP on starter pellets, drying the pellets, layering them with subcoating and enteric coating, mixing with glidants where applicable and filling into capsules.  
   
   
       38 . A method for the prophylaxis or treatment of a clinical condition in a mammal, such as a human, for which a proton pump inhibitor is indicated, which comprises administration of a therapeutically effective amount (S)-pantoprazole magnesium in a dosage form according to  claim 18.